N-(7,9-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-1H-benzimidazole-5-carboxamide | 677338-37-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: N-(7,9-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-1H-benzimidazole-5-carboxamide
• 英文别名: N-(7,9-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-3H-benzimidazole-5-carboxamide
• CAS: 677338-37-3
• 化学式: C₂₀H₁₈N₆O₃
• 分子量: 390.401
• InChiKey: OYLANDUSDVCRTH-UHFFFAOYSA-N

物化性质

• 密度：
  1.53±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2168582A1

  公开（公告）日：2010-03-31

  The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.

  本发明涉及使用2,3-二氢咪唑[1,2-c]喹唑啉化合物，以及含有这种化合物的药物组合物，用于治疗或预防多发性骨髓瘤，作为单一药剂或与其他一个或多个其他活性成分联合使用。
• Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2168583A1

  公开（公告）日：2010-03-31

  The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.

  本发明涉及使用2,3-二氢咪唑[1,2-c]喹唑啉化合物以及含有这种化合物的药物组合物，用于治疗或预防多发性骨髓瘤，作为唯一药剂或与其他一种或多种其他活性成分联合使用。
• Use of substituted 2,3-dihydroimidazo[1,2-C]quinazolines
  申请人：Liu Ningshu

  公开号：US10202385B2

  公开（公告）日：2019-02-12

  The present invention relates to: —use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of cancer; —combinations of a) said compound and b) one or more further active agents; —a pharmaceutical composition comprising said compound as a sole active agent for the treatment of breast cancer; —a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; —use of biomarkers involved in the modification of Bel expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based synergistic combination as defined herein to increase sensitivity and/or to overcome resistance; and —a method of determining the level of a component of one or more of Bcl expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN.

  本发明涉及以下内容：-使用2,3-二氢咪唑并[1,2-c]喹唑啉化合物或含有该化合物的药物组合物作为唯一活性成分，或a)该化合物或含有该化合物的药物组合物和b)一个或多个进一步的活性成分的组合，用于制备用于治疗或预防癌症的药物；-a)该化合物和b)一个或多个进一步的活性成分的组合；-仅含有该化合物作为唯一活性成分的药物组合物，用于治疗乳腺癌；-含有a)该化合物和b)一个或多个进一步的活性成分的药物组合物；-使用涉及Bel表达的修饰、HER家族表达和/或激活、PIK3CA信号传导和/或PTEN丧失的生物标志物来预测癌症患者对该化合物的敏感性和/或耐药性，并提供基于理性的协同组合，以增强敏感性和/或克服耐药性；以及-确定Bcl表达、HER家族表达和/或激活、PIK3CA信号传导和/或PTEN的一个或多个组分的水平的方法。
• Fused azole-pyrimidine derivatives
  申请人：Shimada Mitsuyuki

  公开号：US20060128732A1

  公开（公告）日：2006-06-15

  The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

  本发明涉及杂环融合的唑啉嘧啶衍生物，以及制备它们的方法和含有它们的制药制剂。本发明的杂环融合的唑啉嘧啶衍生物表现出增强的磷脂酰肌醇-3-激酶（PI3K）抑制活性，特别是PI3K-γ抑制活性，并可用于预防和治疗与PI3K和特别是PI3K-γ活性相关的疾病。更具体地说，本发明的唑啉衍生物可用于以下疾病的治疗和预防：炎症和免疫调节性疾病，如哮喘、特应性皮炎、鼻炎、过敏疾病、慢性阻塞性肺病（COPD）、感染性休克、关节疾病、类风湿性关节炎和格雷夫斯病、癌症、心肌收缩力障碍、心力衰竭、血栓栓塞、缺血和动脉硬化。本发明的化合物还可用于肺动脉高压、肾功能衰竭、心脏肥大，以及神经退行性疾病，如帕金森病、阿尔茨海默病、糖尿病和局部缺血，因为这些疾病也与人类或动物主体中的PI3K活性有关。
• FUSED AZOLE-PYRIMIDINE DERIVATIVES
  申请人：Shimada Mitsuyuki

  公开号：US20090270388A1

  公开（公告）日：2009-10-29

  The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

  本发明涉及新型的融合式唑啉嘧啶衍生物、其制备方法和含有它们的药物制剂。本发明的融合式唑啉嘧啶衍生物表现出增强的磷脂酰肌醇-3-激酶（PI3K）抑制活性，特别是对PI3K-γ的抑制活性，可用于预防和治疗与PI3K，特别是PI3K-γ活性相关的疾病。更具体地说，本发明的唑啉嘧啶衍生物可用于以下疾病的治疗和预防：炎症和免疫调节性疾病，如哮喘、特应性皮炎、鼻炎、过敏疾病、慢性阻塞性肺疾病（COPD）、感染性休克、关节疾病、类风湿性关节炎和格雷夫斯病、癌症、心肌收缩功能障碍、心力衰竭、血栓栓塞、缺血和动脉硬化。本发明的化合物还可用于肺动脉高压、肾衰竭、心脏肥大，以及神经退行性疾病，如帕金森病、阿尔茨海默病、糖尿病和局灶性缺血，因为这些疾病也与人类或动物主体中的PI3K活性有关。